Copper Complexes of 8-Aminoquinoline and Uracils as Novel Aromatase Inhibitors

Author(s): Nujarin Sinthupoom, Veda Prachayasittikul, Ratchanok Pingaew, Apilak Worachartcheewan, Supaluk Prachayasittikul*, Somsak Ruchirawat, Virapong Prachayasittikul*

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 8 , 2017

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Graphical Abstract:


Background: Currently, aromatase inhibitors (AIs) have been developed for the treatment of breast cancers and other estrogen-related conditions. However, searching for more and new classes of AIs is being investigated. 8-Aminoquinoline (8AQ) is an interesting scaffold to be explored. In particular, 8AQ as its mixed ligands (5-nitrouracil, 5Nu and 5-iodouracil, 5Iu) metal complexes are potential compounds to be studied.

Objective: Metal complexes of 8AQ-5Nu/5Iu were investigated for aromatase inhibitory activity and cytotoxicity.

Methods: Metal complexes (1-6) and free ligands were evaluated for aromatase inhibitory and cytotoxic activities. Aromatase inhibitory activity of the metal complexes was performed according to a guideline of BD Gentest™ kit using CYP19 enzyme and O-benzyl fluorescein (DBF) as a substrate. Cytotoxic effect of the compounds was tested against normal embryonic lung cell line (MRC) using the MTT assay.

Results: Significantly, copper complexes 3 (IC50 = 0.7 μM) and 6 (IC50 = 1.7 μM) were shown to be active aromatase inhibitors with selectivity indices of 24.74 and16.40, respectively.

Conclusion: Copper complexes of 8AQ-5Nu (3) and of 8AQ-5Iu (6) were highlighted as novel aromatase inhibitors that could be further developed for therapeutic applications.

Keywords: 8-Aminoquinoline, uracil, metal complex, aromatase inhibitor, cytotoxicity, cancer treatment.

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Article Details

Year: 2017
Published on: 19 July, 2017
Page: [880 - 884]
Pages: 5
DOI: 10.2174/1570180813666161103144822
Price: $65

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